Beta-lactamase inhibitors

a technology of beta-lactamase and inhibitor, which is applied in the direction of biocide, antibacterial agents, drug compositions, etc., can solve the problems of increasing the cost of treatment, increasing the mortality of patients, and increasing the risk of infection, so as to improve the survival rate, inhibit beta-lactamase, and improve the effect of antibacterial
US20110294777A1Active Publication Date: 2011-12-01MERCK SHARP & DOHME LLC
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Patent Information

Authority / Receiving Office
US · United States
Patent Type
Applications(United States)
Current Assignee / Owner
MERCK SHARP & DOHME LLC
Publication Date
2011-12-01

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Abstract

Substituted bicyclic beta-lactams of Formula I: (I), are β-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds can be employed with a β-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.
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Description

CROSS-REFERENCE TO RELATED APPLICATIONS

[0001] This application claims the benefit of U.S. Provisional Application No. 61 / 011,533 (filed Jan. 18, 2008), the disclosure of which is hereby incorporated by reference in its entirety.FIELD OF THE INVENTION

[0002] This invention relates to novel beta-lactamase inhibitors and their use against bacterial antibiotic resistance. More particularly, the invention relates to compositions and methods for overcoming bacterial antibiotic resistance.BACKGROUND OF THE INVENTION

[0003] Bacterial antibiotic resistance has become one of the most serious threats to modern health care. Cohen, Science 1992, 257: 1051-1055 discloses that infections caused by resistant bacteria frequently result in longer hospital stays, higher mortality and increased cost of treatment. Neu, Science 1992, 257: 1064-1073 discloses that the need for new antibiotics will continue to escalate because bacteria have a remarkable ability to develop resistance to new agents rendering them...

Claims

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